好色先生

好色先生

Explore the latest content from across our publications

Log In

Forgot Password?
Create New Account

Loading... please wait

Abstract Details

Safety, Tolerability, and Pharmacokinetics of BHV-2100, a First-in-class TRPM3 Antagonist for Pain and Migraine
Pain
S11 - Pain (11:51 AM-12:03 PM)
004

TRPM3 is a calcium-permeable, nonselective TRP channel expressed in somatosensory neurons, including nociceptors. Several lines of evidence, including preclinical and human genetic data, implicate TRPM3 in pain signaling and migraine. BHV-2100 is a first-in-class TRPM3 antagonist in development for pain and migraine that has demonstrated potent pain reversal in preclinical models.

Assess the safety, tolerability, and pharmacokinetics of BHV-2100.

This was a randomized, placebo-controlled, sequential single and multiple ascending dose (SAD/MAD) study. Healthy adults aged 18-55 years were enrolled. SAD participants were randomized 3:1 to single dose BHV-2100 (25, 75, 150, 250, or 500mg) or placebo under fasting conditions; 150mg was also tested with food and famotidine. MAD participants were randomized 3:1 to BHV-2100 (25, 75, 150mg once-daily or 150mg twice-daily) or placebo and treated for 14 days. Safety and pharmacokinetics were evaluated.

In the SAD and MAD cohorts, 39 and 32 participants were treated, respectively. AEs occurring in >1 participant across pooled BHV-2100 SAD doses included dizziness and fatigue, each occurring in 2/30 BHV-2100-treated participants and 0/9 placebo-treated participants. No AEs occurred in >1 participant across BHV-2100 MAD doses. No serious or severe AEs were reported. Most AEs were mild and resolved spontaneously without treatment. No clinically significant trends in vital signs, laboratory values, or ECGs were observed. Plasma concentrations exceeded EC90 after 20 minutes and were sustained above EC90 for several hours at all dose levels. Tmax was 1.5-2 hours; half-life was 8-12 hours. Once-daily 75mg provided plasma concentrations >EC50 over 24 hours; 150mg twice-daily provided >EC90 over 24 hours. Dosing with food or famotidine did not significantly impact pharmacokinetics.

TRPM3 represents a novel target for the treatment of pain and migraine. BHV-2100 demonstrated excellent safety and pharmacokinetics and is being evaluated in clinical trials for pain (EudraCT 2024-512187-57) and migraine (NCT06603623) as a novel non-opioid treatment.

Authors/Disclosures
Volkan Granit, MD
PRESENTER
Dr. Granit has received personal compensation for serving as an employee of Biohaven Pharmaceuticals. Dr. Granit has stock in Biohaven. Dr. Granit has received personal compensation in the range of $10,000-$49,999 for serving as a Faculty Member with University of Miami.
Richard Bertz (Biohaven Pharmaceuticals) Richard Bertz has received personal compensation for serving as an employee of Biohaven Pharmaceuticals. Richard Bertz has stock in Biohaven Pharmaceuticals.
Andrew Lucas, PharmD, MS, MS Dr. Lucas has nothing to disclose.
Eric Ashbrenner Eric Ashbrenner has received personal compensation for serving as an employee of Biohaven. Eric Ashbrenner has stock in Biohaven. An immediate family member of Eric Ashbrenner has stock in Biohaven.
Mary Donohue (Biohaven Pharmaceuticals, Inc.) Mary Donohue has received personal compensation for serving as an employee of Biohaven Pharmaceuticals, Inc.. Mary Donohue has stock in Biohaven Pharmaceuticals, Inc..
Patricia Mydlow (Biohaven) Patricia Mydlow has received personal compensation in the range of $100,000-$499,999 for serving as a Consultant for Biohaven Pharma.
Christopher Jensen, PharmD (Biohaven Pharmaceuticals) Dr. Jensen has received personal compensation for serving as an employee of Biohaven Pharmaceuticals. Dr. Jensen has stock in Biohaven Pharmaceuticals.
Joris Vriens Joris Vriens has received intellectual property interests from a discovery or technology relating to health care.
Thomas Voets (VIB-KU Leuven Center for Brain and Disease Research) Thomas Voets has received intellectual property interests from a discovery or technology relating to health care.
Beth Emerson, MD Dr. Emerson has received personal compensation for serving as an employee of Biohaven. Dr. Emerson has received personal compensation for serving as an employee of Pfizer. Dr. Emerson has stock in Biohaven. Dr. Emerson has stock in Pfizer.
Irfan Qureshi, MD (Biohaven Pharmaceuticals) Dr. Qureshi has received personal compensation for serving as an employee of Biohaven. Dr. Qureshi has stock in Biohaven Pharmaceuticals.
Vladimir Coric Vladimir Coric has received personal compensation for serving as an employee of Biohaven. Vladimir Coric has received personal compensation in the range of $1,000,000+ for serving as an officer or member of the Board of Directors for Bioahven. Vladimir Coric has stock in Biohaven. Vladimir Coric has received intellectual property interests from a discovery or technology relating to health care.